Abacavir (Abacavirum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Means for the treatment of HIV infection

Included in the formulation
  • Abacavir
    pills inwards 
    Bright Pharmaceuticals Operation Sente     China
  • Abacavir
    pills inwards 
    Heterose Labs Limited     India
  • Abacavir
    pills inwards 
    IRVIN 2, LLC     Russia
  • Abacavir
    pills inwards 
    IBA-groups, LLC     Russia
  • Abacavir
    solution inwards 
    ATOLL, LLC     Russia
  • Abacavir Canon
    pills inwards 
    CANONFARMA PRODUCTION, CJSC     Russia
  • Abacavir-ABC
    pills inwards 
    TECHNOLOGY OF DRUGS, LTD.     Russia
  • Ziagen®
    pills inwards 
    VeeV Helsker United Kingdom Limited     United Kingdom
  • Ziagen®
    solution inwards 
    VeeV Helsker United Kingdom Limited     United Kingdom
  • Olitid
    pills inwards 
    FARMSINTEZ, PAO     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    J.05.A.F.06   Abacavir

    Pharmacodynamics:

    An antiviral agent. The analogue of guanosine, the nucleoside reverse transcriptase inhibitor HIV-1 and HIV-2.

    HIV refers to RNA-containing viruses, so for the life cycle it needs to transcribe viral RNA into complementary DNA using its own reverse transcriptase. Abacavir, like natural nucleosides, is phosphorylated by human cell kinases in three steps.At the final stage, it turns into carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTF), capable of competitively integrating into viral DNA and blocking the elongation of the DNA strand by reverse transcriptase, which leads to a halt in the development of the virus. Human DNA polymerase is better than reverse transcriptase of the virus, it discriminates natural nucleotides from their analogues, therefore, carbovir triphosphate is much less integrated into human DNA and has little effect on cells. However, carbovir triphosphate is able to inhibit the synthesis of mitochondrial DNA from host cells, determining its mitochondrial toxicity. The development of HIV resistance to abacavir is due to mutations leading to the ability of reverse transcriptase of the virus to discriminate the active metabolite of abacavir from natural nucleotides. The resistance of HIV to abacavir is developing slowly.

    Pharmacokinetics:When ingested quickly absorbed, bioavailability high - 83% (63-100%). The volume of distribution is 0.83 (0.69-1.03) l / kg, the concentration in the cerebrospinal fluid - 28-33% of that in plasma. Connection with plasma proteins - 50 %. Biotransformation occurs in the liver with the participation of alcohol dehydrogenase,glucuronyl transferase. Half-life is 1 (0.8-1.3) h, intracellular half-elimination (carbovir triphosphate) - 3 hours. Elimination of the kidneys unchanged - 81%, in the form of metabolites - 1.6% and with feces - 16 %. Do not cumulate.
    Indications:

    HIV infection (as part of combined antiretroviral therapy).

    ICD-10

    I.B20-B24   Disease caused by the human immunodeficiency virus [HIV]

    Contraindications:

    Hypersensitivity, children under 3 months.

    Carefully:Diseases of the liver. Pregnancy and lactation.
    Pregnancy and lactation:Pregnancy: category C on the recommendation of the FDA.

    HIV-infected women are advised in all situations to avoid breastfeeding in order to prevent HIV transmission to their children. Women who use abacavir, it is also not recommended to breast-feed the baby.

    Dosing and Administration:Inside 300 mg 2 times a day, regardless of food intake at strictly defined hours. The maximum dose is 600 mg per day. Children from 3 months to 12 years - 8 mg / kg twice a day; 12-18 years - 300 mg twice a day.
    Side effects:

    Hypersensitivity reaction: usually in the first 6 weeks of treatment. Toxic epidermal necrolysis, Stevens-Johnson syndrome.

    Nervous system: fatigue, headache, insomnia.

    Hemopoietic system: lymphopenia.

    Digestive system: diarrhea, nausea, vomiting, loss of appetite, abdominal pain.

    Liver and pancreas: hepatomegaly, steatosis. Lactic Acidosis, up to a lethal outcome (especially in pregnant women). Pancreatitis.

    Musculoskeletal system: pain in muscles, cramps, weakness. Obesity (the deposition of adipose tissue on the face, body, chest - Cushing's syndrome).

    Other: dyspnea, fever, malaise, swelling.

    Overdose:Symptoms: anxiety, dizziness, headache, drowsiness, convulsions, nausea, vomiting and other signs of increased side effects.

    Treatment symptomatic.

    Interaction:

    The likelihood of clinically significant interactions of abacavir with other drugs is very low.

    Amprenavir and abacavir when combined, the effect and the risk of toxicity are mutually reinforcing, caution is necessary when prescribing.

    Ethanol slows metabolism, increases the maximum concentration and half-life of abacavir.

    Co-administration with methadone may reduce the maximum concentration of abacavir. The time for reaching the maximum concentration increases by 1 hour.

    Abacavir increases the average systemic methadone clearance by 22%, so an increase in the dose of methadone may be required.

    Rifampicin, tipranavir, phenytoin, phenobarbital when combined, reduce the plasma concentration of abacavir.

    Possible competition for alcohol dehydrogenase with drugs metabolized with its participation (retinoids).

    Special instructions:

    The resistance of some strains of HIV-1 to abacavir is probably related to changes in the genotype in a certain codon region of reverse transcriptase (codons M184V, K65R, L74V, Y115F, M184V and L74V). In vitro, cross-resistance of HIV-1 to abacavir and other nucleoside reverse transcriptase inhibitors has also been documented. The development of cross-resistance of HIV to HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors is unlikely.

    When taking abacavir, you need to monitor the number of CD4 + lymphocytes, viral load, peripheral blood, symptoms of hypersensitivity.

    Do not use abacavir in monotherapy, it is advisable to appoint as part of a highly active combination therapy.

    For antiretroviral prophylaxis of transplacental transmission of HIV from mother to the fetus, it is recommended that zidovudine and nevirapine (more effective).

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